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Assay Detail

CHEMBL950102

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Agonist activity at human PPARalpha expressed in monkey CV1 cells by transactivation assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CV-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Peroxisome proliferator-activated receptor alpha (CHEMBL239)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a novel class of 1,3-dioxane-2-carboxylic acid derivatives as subtype-selective peroxisome proliferator-activated receptor alpha (PPARalpha) agonists.
Aoki T, Asaki T, Hamamoto T, Sugiyama Y, Ohmachi S, Kuwabara K, Murakami K, Todo M.
Bioorg Med Chem Lett (2008) 18 : 2128 -2132
PubMed 18280733 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 6.02 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL271873 1 7.52
CHEMBL447533 1 7.52
CHEMBL270835 1 7.00
CHEMBL401811 1 6.52
CHEMBL401616 1 6.52
CHEMBL401712 1 5.52
CHEMBL256013 1 5.52
CHEMBL404439 1 5.52
CHEMBL270836 1 5.52
CHEMBL264374 BEZAFIBRATE 3.0 1 4.52
CHEMBL981 FENOFIBRIC ACID 4.0 1 4.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL271873 EC50 = 30.0 nM 7.52
CHEMBL447533 EC50 = 30.0 nM 7.52
CHEMBL270835 EC50 = 100.0 nM 7.00
CHEMBL401811 EC50 = 300.0 nM 6.52
CHEMBL401616 EC50 = 300.0 nM 6.52
CHEMBL401712 EC50 = 3000.0 nM 5.52
CHEMBL256013 EC50 = 3000.0 nM 5.52
CHEMBL404439 EC50 = 3000.0 nM 5.52
CHEMBL270836 EC50 = 3000.0 nM 5.52
CHEMBL264374 BEZAFIBRATE EC50 = 30000.0 nM 4.52
CHEMBL981 FENOFIBRIC ACID EC50 = 30000.0 nM 4.52